Target intelligence / Profile preview

Gastrin-releasing peptide (GRP)

Target
GRP
Molecular classification
Neuropeptide, Peptide hormone, Regulatory peptide, Bombesin-like peptide
01

Overview

Gastrin-releasing peptide (GRP) is a 27-amino acid neuropeptide and regulatory peptide hormone encoded by the *GRP* gene.[2][4][6] It is synthesized as a larger precursor (preproGRP) and processed to produce GRP and neuromedin C fragments.[4] GRP has significant physiological roles in the regulation of gastrointestinal and central nervous system functions, including stimulation of gastrin and other hormone release, promoting gastric acid secretion, influencing gastrointestinal motility, and stimulating cell proliferation.[3][4][6] Its main mechanism of action is through activation of the gastrin-releasing peptide receptor (GRPR, also known as BB2), a class A G protein-coupled receptor, which is the true therapeutic target in most drug development programs, especially for cancer and pruritus.[1][4] Elevated expression of the GRP/GRPR axis is implicated in several cancers, making pro-GRP and GRP themselves potential biomarkers for diagnosis or monitoring.[3][4]

Other names
Gastrin Releasing PeptideGRPBombesin-like peptideNeuromedin C (for GRP(18-27) decapeptide fragment)
02

Mechanism of action

Acts via binding and activating the gastrin-releasing peptide receptor (GRPR), a G protein-coupled receptor Induces intracellular signaling leading to hormone secretion and cell signaling events

03

Biological functions

Regulation of gastric acid secretionStimulation of gastrin releaseRegulation of gastrointestinal motilityPancreatic secretionLung developmentNeurotransmissionCell proliferationChemoattraction in immune system cells
04

Disease associations

Cancer (due to proliferative signaling and GRP/GRPR axis in tumors)Gastrointestinal disordersPulmonary disordersPruritus/itch (via central mechanisms)
05

Safety considerations

GRP has mitogenic effects: aberrant activation in tumors could support uncontrolled cell growthModulation in the CNS may affect body temperature and metabolism (based on animal studies)
06

Interacting drugs

No direct drugs, but antagonists targeting GRP receptor (GRPR)

1 more in the full profile.

07

Biomarkers

Elevated GRP or pro-GRP as a biomarker in certain cancers (for example, small cell lung cancer)Used to select patients or monitor efficacy in oncology trials

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